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B.-R. Choi, K.K. Karna, Y.-S. Shin, S.-W. Lee, C.-Y. Kim, H.-K. Kim, J.-K. Park, PO-01-018 Comparative Pharmacokinetic and Bioavailability Studies of Monotropein, Kaempferol 3-O-glucoside and Quercetin 4'-O-glucoside after Oral and Intraveneous Administration of MOTILIPERM in Rats, The Journal of Sexual Medicine, Volume 16, Issue Supplement_2, May 2019, Pages S53–S54, https://doi.org/10.1016/j.jsxm.2019.03.181
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Objective
The present study was designed to validate liquid chromatography tandem mass spectrometry (LC-MS/MS) method for pharmacokinetic and bioavailability investigation of monotropein, kaempferol 3-O-glucoside and quercetin 4'-O-glucoside in MOTILIPERM following oral and intravenous administration of its extract.
Methods
MOTILIPERM was prepared as a mixture of extracts of three medicinal herbs roots from Morinda officinalis How (Rubiaceae), seeds of Cuscuta chinensis Lamark (Convolvulaceae) and outer scales of Allium cepa Linnaeus (Liliaceae). After intravenous or oral administration of MOTILIPERM at 20 or 400 mg/kg to rats respectively, the plasma concentrations of monotropein, kaempferol 3-O-glucoside and quercetin 4'-O-glucoside were simultaneously determined in rats. Simultaneous determination of monotropein, kaempferol 3-O-glucoside and quercetin 4'-O-glucoside of MOTILIPERM by liquid chromatography tandem mass spectrometry (LC-MS/MS) method was fully validated and successfully applied to pharmacokinetics and bioavailability study.
Results
Pharmacokinetic parameters of monotropein in rats were AUCinf 20020.44 ± 3944.67 and 11915.53 ± 1190.91 min·ng/mL; Cmax 286.99 ± 38.37 and 56.23 ± 9.02 ng/mL for intravenous and oral administration, respectively. Pharmacokinetic parameters of kaempferol 3-O-glucoside in rats were AUCinf 287.86 ± 126.17 min·ng/mL and not estimated; Cmax 5.80 ± 1.87 and 1.24 ± 0.41 ng/mL for intravenous and oral administration, respectively. Pharmacokinetic parameters of quercetin 4'-O-glucoside in rats were AUCinf 511.38 ± 248.11 and 481.44 ± 65.72 min·ng/mL; Cmax 10.72 ± 2.70 and 2.83 ± 0.34 ng/mL for intravenous and oral administration, respectively. The absolute bioavailability of monotropein and quercetin 4'-O-glucoside for oral administration are evaluated and calculated as 3.0% and 4.7%, respectively. The absolute bioavailability of kaempferol 3-O-glucoside was not calculated because the elimination rate constant cannot be estimated.
